title: Formulation and evaluation of metoclopramide solid lipid nanoparticles for rectal suppository.
abstract: OBJECTIVE
  The purpose of this study was to formulate and characterize metoclopramide solid lipid nanoparticles (MCP-SLNs) and incorporating it into suppository bases for treatment of nausea and vomiting, produced with chemotherapeutic agents, using one dose per day.
  
  
  METHODS
  MCP-SLNs was prepared using high shear homogenization (hot homogenization) technique using different surfactants (tween 80, poloxamer 407, poloxamer 188 and cremophore) in two different concentrations (2.5% and 5%) then solid lipid nanoparticle (SLN), whose release percentage above 50%, was incorporated into suppository for treatment of nausea and vomiting. The prepared SLN and suppositories were then evaluated and characterized.
  
  
  RESULTS
  Formulation of poloxamer 407 with compritol and drug (F9) produced highest in-vitro % release (80%). Transmission electron microscopy showed that SLN had round and spherical shape in form of solid dispersion or drug-enriched core. Particle size analysis of SLN showed a size range of 24.99-396.8 nm. Negative zeta potential proves complete drug entrapment. In-vivo study of MCP-SLN suppositories produced the same %GE as the market metoclopramide (MCP) suppository (Primperan) with sustained release effect.
  
  
  CONCLUSIONS
  MCP-SLN suppositories (formula F) can reverse decrease in %GE because of emesis with sustained release effect. So it succeeded to be an alternative to MCP suppositories with no multiple dosing.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy and Biotechnology, German University in Cairo, GUC, Cairo, Egypt.
authors.forename: Radwa A
authors.initials: RA
authors.lastname: Mohamed
authors.forename: Haidy A
authors.initials: HA
authors.lastname: Abass
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Attia
authors.forename: Ola A
authors.initials: OA
authors.lastname: Heikal
mesh_terms: D000285:Administration, Rectal; D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage* / Q000627:therapeutic use; D003692:Delayed-Action Preparations; D018492:Dopamine Antagonists / Q000008:administration & dosage; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D005227:Fatty Acids; D005260:Female; D005746:Gastric Emptying; D008787:Metoclopramide / Q000008:administration & dosage* / Q000627:therapeutic use; D053758:Nanoparticles; D009325:Nausea / Q000188:drug therapy; D010316:Particle Size; D020442:Poloxamer; D051381:Rats; D013488:Suppositories / Q000592:standards; D013501:Surface-Active Agents; D014839:Vomiting / Q000188:drug therapy
chemical_list: D000932:Antiemetics; D003692:Delayed-Action Preparations; D018492:Dopamine Antagonists; D004337:Drug Carriers; D005227:Fatty Acids; D013488:Suppositories; D013501:Surface-Active Agents; D020442:Poloxamer; C086409:glyceryl behenate; D008787:Metoclopramide
keywords: gastric emptying percent; high-shear homogenization; metoclopramide; solid lipid nanoparticle-loaded suppositories; solid lipid nanoparticles